Free shipping on all orders over $ 500

AZD4547

Cat. No. M1721
AZD4547 Structure
Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 280 In stock
100mg USD 380 In stock
Bulk Inquiry?

Quality Control
Biological Activity

AZD4547 is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.

Protocol
Cell Experiment
Cell lines MCF-7 cell line
Preparation method In vitro cell-cycle and apoptotic induction analysis
Cell lines were incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells were fixed with 70% ethanol and then incubated with propidium iodide/RNase A (Sigma) labeling solution. Cell-cycle profiles were assessed with a FACSCalibur instrument and CellQuest analysis software (Becton Dickinson). For apoptotic analysis, cells and media were gently harvested and centrifuged, followed by washing of cell pellets. Cells were then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake according to the manufacturer's instructions (Abcam). The proportion of cells staining positive for Annexin V were then assessed with a FACSCalibur instrument and quadrant sorting was done by CellQuest analysis software (Becton Dickinson).
Concentrations 0.003~1 μM
Incubation time 72 h
Animal Experiment
Animal models nude mice bearing established Calu-6 human tumor xenografts
Formulation formulated in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water
Dosages 1.5–50 mg/kg once daily or twice daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 463.58
Formula C26H33N5O3
CAS Number 1035270-39-3
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance.
Chell et al. Oncogene. 2012 Aug 6. PMID: 22869148.

AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family.
Gavine et al. Cancer Res. 2012 Apr 15;72(8):2045-56. PMID: 22369928.

Related EGFR/HER2 Products
Anlotinib

Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.

Cetuximab

Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD.

EAI045

EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.

Gefitinib HCl

Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.

Erlotinib

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD4547 supplier, EGFR/HER2, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.